abstract

• The bioavailability of two oral forms of cyclosporin A (Sandimmun and Neoral™) was assessed in 10 children with end stage renal disease (ESRD) on dialysis. The study was performed at steady state according to a randomized, double blind, cross-over design, allowing a one month washout period between treatments. Each patient received 2.5 mg/kg (po) of cyclosporin every 12 h, either Sandimmun or Neoral, and serum concentrations were determined repeatedly during a 24 h period after the 5th dose of cyclosporin. Serum concentration against time curves were constructed and bioavailability, expressed as AUC and Cmax, observed with each formulation, was compared. AUC was 90%25 and Cmax was 130%25 higher with Neoral than Sandimmun. Considering that the international accepted criteria for bioequivalence allow 20%25 variation in AUC and Cmax, it appears that Neoral and Sandimmun are not bioequivalent in children with ESRD. Notwithstanding, there were no significant differences in trough levels between formulations. We conclude that, if trough levels are the sole source of information for dosing design, Neoral can be substituted with Sandimmun on a 1:1 basis. However, a 1:1 substitution does not appear to be adequate when AUC is used in children with ESRD.

authors

• Campos A.E.
• Castañeda G.
• Gomez C.
• Medeiros M.
• Muñoz R.
• Pérez-Urizar J.
• Ramirez E.
• Romero B.
• Saldaña M.Y.
• Velasquez L.F.

publication date

• 1998-01-01

published in

• Proceedings of the Western Pharmacology Society  Journal

start page

• 281

end page

volume

• 41